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'Gym pill' trips fat-burning gene

Oswizle

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Last Updated: Sunday, 29 April 2007, 23:42 GMT 00:42 UK

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'Gym pill' trips fat-burning gene

The aim of the pill is to prevent disease rather than build muscles
US scientists have devised a drug that can switch on a gene to burn body fat, offering hope of an exercise pill.
Mice given the drug burned off fat, even when they did not exercise, and were resistant to weight gain despite a high-fat diet.

The ultimate use would be to treat people at risk of obesity-related diseases like diabetes, rather than offer a "no-work six-pack" pill.

The Salk Institute team presented their work at Experimental Biology 2007.

Although this might become an 'exercise pill', it is unlikely to provide all the other benefits of real physical exercise

UK expert Dr Fredrik Karpe

The drug mimics normal fat and chemically triggers a gene switch called PPAR-delta.

Turning on this switch activates the same fat-burning process that occurs during exercise.

Lead researcher Dr Ronald Evans believes the same will occur in humans.

Human trials

UK expert Dr Fredrik Karpe, from the Oxford Centre for Diabetes, Endocrinology and Metabolism, is hoping to test this in the near future.

Commenting on the work, he said: "There has never been a method to 'medically' switch on fat burning before.

"The finding that PPAR-delta co-ordinates this process, not only by switching on fat burning, but also to rebuild the muscle in a way making it more fit for fat burning, is of major interest, not least as a completely novel approach for the treatment of the metabolic derangements accompanying obesity."

But he cautioned; "Although this might become an 'exercise pill', it is unlikely to provide all the other benefits of real physical exercise."
 
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Rudolph J, Chen L, Majumdar D, Bullock WH, Burns M, Claus T, Dela Cruz FE, Daly M, Ehrgott FJ, Johnson JS, Livingston JN, Schoenleber RW, Shapiro J, Yang L, Tsutsumi M, Ma X. Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy. J Med Chem. 2007 Mar 8;50(5):984-1000. [view PubMed record (17274610)]

Matches:

* [TITLE] Indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail groups, a new class of potent PPAR alpha/gamma/delta pan agonists: synthesis, structure-activity relationship, and in vivo efficacy.

* Compounds that simultaneously activate the three peroxisome proliferator-activated receptor (PPAR) subtypes alpha, gamma, and delta hold potential to address the adverse metabolic and cardiovascular conditions associated with diabetes and the metabolic syndrome.

* While most of the tail group modifications imparted potent PPAR delta agonist activity, improvement of PPAR alpha and gamma activity required the introduction of new heterocyclic substituents that were not known in the PPAR literature.

* Systematic optimization led to the discovery of 4-thiazolyl-phenyl derivatives with potent PPAR alpha/gamma/delta pan agonistic activity.

* [MeSH] chemical synthesis. chemical synthesis. chemical synthesis. agonists. agonists. agonists. chemical synthesis. Acetic Acids. chemistry. pharmacology. Animals. Apolipoprotein A-I. genetics. Cell Line. Cricetinae. Female. Humans. Hyperlipidemias. drug therapy. Hypoglycemic Agents. chemistry. pharmacology. Indans. chemistry. pharmacology. Lipids. blood. Male. Mice. Mice, Transgenic. PPAR alpha. genetics. PPAR delta. PPAR gamma. genetics. Radioligand Assay. Rats. Rats, Zucker. Solubility. Stereoisomerism. Structure-Activity Relationship. Trans-Activation (Genetics). Triazoles. chemistry. pharmacology
 
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Cantin LD, Liang S, Ogutu H, Iwuagwu CI, Boakye K, Bullock WH, Burns M, Clark R, Claus T, delaCruz FE, Daly M, Ehrgott FJ, Johnson JS, Keiper C, Livingston JN, Schoenleber RW, Shapiro J, Town C, Yang L, Tsutsumi M, Ma X. Indanylacetic acid derivatives carrying aryl-pyridyl and aryl-pyrimidinyl tail groups--new classes of PPAR gamma/delta and PPAR alpha/gamma/delta agonists. Bioorg Med Chem Lett. 2007 Feb 15;17(4):1056-61. [view PubMed record (17157013)]

Matches:

* [TITLE] Indanylacetic acid derivatives carrying aryl-pyridyl and aryl-pyrimidinyl tail groups--new classes of PPAR gamma/delta and PPAR alpha/gamma/delta agonists.

* The indanylacetic acid structural motif has proven useful in the generation of potent and tunable PPAR ligands.
 
Very interesting, but PPARdelta agonism has links to cancer, and fairly strong links at that. The relationship isn't fully understood, so we probably won't be messing with PPARdelta until the relationship becomes clearer.

PPARgamma agonism can create new fat cells, which is obviously not good.

So in general, activation of certain specific PPARs or all three together may not be a good thing. Now, if you have drugs specifically designed to activate certain specific PPARs without negative side effects, then that's another story.

But the trick is to agonize certain PPARs, while downregulating others, for the greatest positive effects on metabolism.
 
I should also add that things also depend on phenotype, insulin resistance, etc., which further complicate things.

Going back to PPARgamma, for example, its agonism may be beneficial for someone with insulin resistance, but not so beneficial for the healthy athlete.

Very complicated stuff.
 
Sir Savage said:
I should also add that things also depend on phenotype, insulin resistance, etc., which further complicate things.

Going back to PPARgamma, for example, its agonism may be beneficial for someone with insulin resistance, but not so beneficial for the healthy athlete.

Very complicated stuff.
Click to expand...

good thing you guys are around to do the dirty work then! just let us have the amazing product of your hard work :food: :head:
 
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